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Assay Detail

CHEMBL858092

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Potency against cloned human alpha 1B adrenoceptor expressed in rat-1 fibroblasts.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
Bishop MJ, Berman J, Bigham EC, Garrison DT, Gobel MJ, Hodson SJ, Irving PE, Liacos JA, Minick DJ, Navas F, Saussy DL, Speake JD.
Bioorg Med Chem Lett (2001) 11 : 2871 -2874
PubMed 11597419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 7.19 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414185 1 9.40
CHEMBL95523 1 8.80
CHEMBL95565 1 7.90
CHEMBL99559 1 7.60
CHEMBL98243 1 7.20
CHEMBL13852 CIRAZOLINE 2.0 1 7.20
CHEMBL95333 1 7.10
CHEMBL100198 1 7.10
CHEMBL95398 1 7.10
CHEMBL318544 1 7.10
CHEMBL98016 1 6.90
CHEMBL329928 1 6.80
CHEMBL99362 1 6.70
CHEMBL97044 1 6.60
CHEMBL450018 1 6.60
CHEMBL95245 1 6.50
CHEMBL421011 1 5.70
CHEMBL329272 1 -
CHEMBL320419 1 -
CHEMBL432192 1 -
CHEMBL761 NAPHAZOLINE 4.0 1 -
CHEMBL98769 1 -
CHEMBL320910 1 -
CHEMBL98921 1 -
CHEMBL100383 1 -
CHEMBL762 OXYMETAZOLINE 4.0 1 -
CHEMBL319553 1 -
CHEMBL96988 1 -
CHEMBL97859 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414185 EC50 = 0.3981 nM 9.40
CHEMBL95523 EC50 = 1.585 nM 8.80
CHEMBL95565 EC50 = 12.59 nM 7.90
CHEMBL99559 EC50 = 25.12 nM 7.60
CHEMBL98243 EC50 = 63.1 nM 7.20
CHEMBL13852 CIRAZOLINE EC50 = 63.1 nM 7.20
CHEMBL95333 EC50 = 79.43 nM 7.10
CHEMBL100198 EC50 = 79.43 nM 7.10
CHEMBL95398 EC50 = 79.43 nM 7.10
CHEMBL318544 EC50 = 79.43 nM 7.10
CHEMBL98016 EC50 = 125.89 nM 6.90
CHEMBL329928 EC50 = 158.49 nM 6.80
CHEMBL99362 EC50 = 199.53 nM 6.70
CHEMBL97044 EC50 = 251.19 nM 6.60
CHEMBL450018 EC50 = 251.19 nM 6.60
CHEMBL95245 EC50 = 316.23 nM 6.50
CHEMBL421011 EC50 = 1995.26 nM 5.70
CHEMBL329272 EC50 < 5011.87 nM -
CHEMBL320419 EC50 < 5011.87 nM -
CHEMBL432192 EC50 < 5011.87 nM -
CHEMBL761 NAPHAZOLINE EC50 < 5011.87 nM -
CHEMBL98769 EC50 < 5011.87 nM -
CHEMBL320910 EC50 < 5011.87 nM -
CHEMBL98921 EC50 < 5011.87 nM -
CHEMBL100383 EC50 < 5011.87 nM -
CHEMBL762 OXYMETAZOLINE EC50 < 5011.87 nM -
CHEMBL319553 EC50 < 5011.87 nM -
CHEMBL96988 EC50 < 5011.87 nM -
CHEMBL97859 EC50 < 5011.87 nM -